WO2003029199A1 - Benzene derivatives, process for preparing the same and use thereof - Google Patents

Benzene derivatives, process for preparing the same and use thereof Download PDF

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Publication number
WO2003029199A1
WO2003029199A1 PCT/JP2002/009995 JP0209995W WO03029199A1 WO 2003029199 A1 WO2003029199 A1 WO 2003029199A1 JP 0209995 W JP0209995 W JP 0209995W WO 03029199 A1 WO03029199 A1 WO 03029199A1
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WO
WIPO (PCT)
Prior art keywords
hydrocarbyl
hydrogen
heterocyclic group
benzene derivatives
preparing
Prior art date
Application number
PCT/JP2002/009995
Other languages
French (fr)
Japanese (ja)
Other versions
WO2003029199A9 (en
Inventor
Takahiro Matsumoto
Masataka Yamamoto
Hiroshi Nagabukuro
Manabu Mochizuki
Original Assignee
Takeda Chemical Industries, Ltd.
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Publication date
Application filed by Takeda Chemical Industries, Ltd. filed Critical Takeda Chemical Industries, Ltd.
Priority to US10/489,621 priority Critical patent/US20040259912A1/en
Priority to EP02768103A priority patent/EP1437344A4/en
Priority to JP2003532453A priority patent/JPWO2003029199A1/en
Publication of WO2003029199A1 publication Critical patent/WO2003029199A1/en
Publication of WO2003029199A9 publication Critical patent/WO2003029199A9/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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Abstract

Novel benzene derivatives represented by the general formula (|), which exhibit vanilloid receptor agonism and are useful as preventive and therapeutic drugs for pollakisuria and urinary incontinence, analgesic, or the like: (|) wherein R1, R4 and R6 are each independently hydrogen, halogeno, or hydrocarbyl; R2 is hydrocarbyl or a heterocyclic group; R3 is hydrocarbyl, NR7’R7, or OR8 (wherein R7’ is hydrogen or hydrocarbyl and R7 is a non-aromatic group, or alternatively R7’ and R7 together with the nitrogen atom adjacent thereto may form a ring; and R8 is hydrocarbyl or a heterocyclic group); R5 is hydrocarbyl or a heterocyclic group (except quinolyl) and R5’ is hydrogen or hydrocarbyl, or R5 and R5’ together with the nitrogen atom adjacent thereto may form a ring; and R5’’ is hydrogen or hydrocarbyl.
PCT/JP2002/009995 2001-09-28 2002-09-27 Benzene derivatives, process for preparing the same and use thereof WO2003029199A1 (en)

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US10/489,621 US20040259912A1 (en) 2001-09-28 2002-09-27 Benzine derivatives, process for preparing the same and use thereof
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